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Assay Detail

CHEMBL3820775

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of oseltamivir-resistant Influenza A virus A/WSN/1933(H1N1) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Influenza A virus (A/WSN/1933(H1N1))
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuraminidase (CHEMBL6135)
Type SINGLE PROTEIN
Organism Influenza A virus

Publication

Peramivir Phosphonate Derivatives as Influenza Neuraminidase Inhibitors.
Wang PC, Fang JM, Tsai KC, Wang SY, Huang WI, Tseng YC, Cheng YS, Cheng TJ, Wong CH.
J Med Chem (2016) 59 : 5297 -5310
PubMed 27167096 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 9.11 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139367 PERAMIVIR ANHYDROUS 4.0 1 10.15
CHEMBL3818436 1 9.52
CHEMBL674 OSELTAMIVIR CARBOXYLATE -1.0 1 9.40
CHEMBL3819487 1 9.30
CHEMBL222813 ZANAMIVIR 4.0 1 9.22
CHEMBL3819617 1 9.22
CHEMBL3819450 1 9.05
CHEMBL3818211 1 9.00
CHEMBL3819314 1 8.82
CHEMBL3818553 1 8.80
CHEMBL3817914 1 8.54
CHEMBL3819492 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139367 PERAMIVIR ANHYDROUS IC50 = 0.07 nM 10.15
CHEMBL3818436 IC50 = 0.3 nM 9.52
CHEMBL674 OSELTAMIVIR CARBOXYLATE IC50 = 0.4 nM 9.40
CHEMBL3819487 IC50 = 0.5 nM 9.30
CHEMBL222813 ZANAMIVIR IC50 = 0.6 nM 9.22
CHEMBL3819617 IC50 = 0.6 nM 9.22
CHEMBL3819450 IC50 = 0.9 nM 9.05
CHEMBL3818211 IC50 = 1.0 nM 9.00
CHEMBL3819314 IC50 = 1.5 nM 8.82
CHEMBL3818553 IC50 = 1.6 nM 8.80
CHEMBL3817914 IC50 = 2.9 nM 8.54
CHEMBL3819492 IC50 = 5.2 nM 8.28